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首页> 外国专利> P-GP RADIOTRACERS FOR IMAGING AS BIOMARKER INVOLVED IN ONSET OF NEURODEGENERATIVE DISEASES

P-GP RADIOTRACERS FOR IMAGING AS BIOMARKER INVOLVED IN ONSET OF NEURODEGENERATIVE DISEASES

机译：P-GP放射性示踪剂，可作为涉及神经退行性疾病发病的生物标记物进行成像

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The invention includes a new class of radiolabeled compounds of formula I able to bind P-glycoprotein with high affinity and selectivity. The protein prevents accumulation in the brain of a wide range of drugs and, changes in P-gp expression and function, are also believed to occur in several neurological disorder, such as Alzheimer's disease (AD). Indeed, it is widely reported that decreased expression of P- gp and/or activity at the BBB level could cause accumulation of I3- amyloid plaques, the main hallmark of AD onset. 13-amyloid is a P-gp substrate, and these results support the importance of P-gp in the clearance of 13-amyloid peptide from brain parenchyma. For this reason, P-gp can be considered a useful biomarker for the early diagnosis of neurodegeneration. There is considerable interest in the development of P-gp PET radiotracers for imaging expression and function of P-gp. Formula I wherein the compound is labeled with an isotope selected from H, 11C14C, 13N, 150 18F19F, 75Br, 76Br, 79Br.
机译：本发明包括一类新的放射性标记的式I化合物，其能够以高亲和力和选择性结合P-糖蛋白。该蛋白质可防止多种药物在大脑中蓄积，并且据信P-gp表达和功能的变化也发生在几种神经系统疾病中，例如阿尔茨海默氏病（AD）。确实，广泛报道了BBB水平P-gp表达降低和/或活性降低可能导致I3-淀粉样斑块的积累，这是AD发作的主要标志。 13-淀粉样蛋白是P-gp的底物，这些结果支持P-gp在清除脑实质中13-淀粉样蛋白肽方面的重要性。因此，可以将P-gp视为早期诊断神经变性的有用生物标记。对用于成像表达和功能的P-gp PET放射性示踪剂的研究引起了极大的兴趣。其中化合物用选自H，11 C 14 C， 13 N，150 18 F < / Sub> 19 F， 75 Br， 76 Br， 79 Br。

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